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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Further sesquiterpenoids from the rhizomes of Homalomena occulta and their anti-inflammatory activity
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Further sesquiterpenoids from the rhizomes of Homalomena occulta and their anti-inflammatory activity

机译:来自Homalomena orculta的根茎和它们的抗炎活动的进一步Sesquiterpenoids

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摘要

The rhizomes of Homalomena occulta are called Qian-nian-jian in Traditional Chinese Medicine (TCM), which is widely consumed in China owing to its health benefits for the treatment of rheumatoid arthritis and for strengthening tendons and bones. A phytochemical investigation on this famous TCM yielded 19 sesquiterpenoids (1-19) with various carbocyclic skeletons including isodaucane (2, 8, and 9), guaiane (3), eudesmane (4 and 10-15), oppositane (5, 16, and 17), and aromadendrane (18 and 19) types. The structures of new compounds, Homalomenins A-E (1-5), were determined by diverse spectroscopic data. Compound 1 possessed a rare sesquiterpenoid skeleton and compound 5 represented the first example of 1,4-oxa-oppositane sesquiterpenoid. These isolates were evaluated for their inhibitory effects on COX-2 mRNA, COX-2 protein expression, and prostaglandin E2 (PGE2) production in Raw264.7 cells, which demonstrated that compounds 5, 18, 19 showed potent anti-inflammatory activity by suppressing LPS-induced COX-2 expression and PGE2 production in a dosedependent manner.
机译:Homalomena Occulta的根茎被称为中医药(TCM)的钱剑,由于其健康益处,为治疗类风湿性关节炎和加强肌腱和骨骼而广泛消耗。对这个着名的TCM的植物化学研究产生了19个Sesquiterpenoids(1-19),各种碳环骨骼(1-19),包括异琥珀(2,8和9),巨莲(3),Eudesmane(4和10-15),对立(5,16, 17),和芳香丁烷(18和19)类型。通过不同的光谱数据测定新化合物的结构Homalomenins A-E(1-5)。化合物1具有稀有倍二萜骨架骨架,化合物5表示1,4-氧气 - 对立筛窦的第一实例。评估这些分离株的抑制作用对RAW264.7细胞中的COX-2 mRNA,COX-2蛋白表达和前列腺素E2(PGE2)产生的抑制作用,其证明了化合物5,18,19通过抑制显示有效的抗炎活性LPS诱导的COX-2表达和PGE2以依赖性方式产生。

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